title: Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
abstract: Histone deacetylase inhibitors (HDACIs) offer a promising strategy for cancer therapy. The discovery of potent ferulic acid-based HDACIs with hydroxamic acid or 2-aminobenzamide group as zinc binding group was reported. The halogeno-acetanilide was introduced as novel surface recognition moiety (SRM). The majority of title compounds displayed potent HDAC inhibitory activity. In particular, FA6 and FA16 exhibited significant enzymatic inhibitory activities, with IC50 values of 3.94 and 2.82 μM, respectively. Furthermore, these compounds showed moderate antiproliferative activity against a panel of human cancer cells. FA17 displayed promising profile as an antitumor candidate. The results indicated that these ferulic acid derivatives could serve as promising lead compounds for further optimization.
authors.affiliation: School of Medicine, Xi'an Jiaotong University, No. 76, Yanta West Road, Xi'an, Shaanxi Province 710061, PR China.
authors.forename: Fang
authors.initials: F
authors.lastname: Wang
authors.forename: Wen
authors.initials: W
authors.lastname: Lu
authors.forename: Tao
authors.initials: T
authors.lastname: Zhang
authors.forename: Jinyun
authors.initials: J
authors.lastname: Dong
authors.forename: Hongping
authors.initials: H
authors.lastname: Gao
authors.forename: Pengfei
authors.initials: P
authors.lastname: Li
authors.forename: Sicen
authors.initials: S
authors.lastname: Wang
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003373:Coumaric Acids / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D062105:Molecular Docking Simulation; D017434:Protein Structure, Tertiary
chemical_list: D000970:Antineoplastic Agents; D003373:Coumaric Acids; D056572:Histone Deacetylase Inhibitors; C004999:ferulic acid; D006655:Histone Deacetylases
keywords: Anticancer; Ferulic acid; HDAC inhibitor; Histone deacetylase